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MK-6884, a positive allosteric modulator (PAM) of M4 muscarinic receptors, exhibits a high affinity (Ki = 0.19 nM). It is a valuable compound for the investigation of neurodegenerative diseases. Additionally, MK-6884 can be efficiently radiolabeled with carbon-11, enabling its use as a PET imaging agent.
Description | MK-6884, a positive allosteric modulator (PAM) of M4 muscarinic receptors, exhibits a high affinity (Ki = 0.19 nM). It is a valuable compound for the investigation of neurodegenerative diseases. Additionally, MK-6884 can be efficiently radiolabeled with carbon-11, enabling its use as a PET imaging agent. |
In vitro | MK-6884 (compound 13; 0-22 μM) functions as a positive allosteric modulator (PAM) of acetylcholine (ACh) in a cell-based calcium (Ca 2+) mobilization assay, with an effective concentration (EC 50) of 27 nM[1]. |
In vivo | [11 C]MK-6884 (compound 13), with a non-displaceable binding potential (BP_ND) of 0.83, effectively penetrates the blood-brain barrier and targets M4 receptors in the rhesus monkeys' brain, as indicated by its distribution following a single intravenous dose of approximately 185 MBq, under 2 μg[1]. |
Molecular Weight | 411.509 |
Formula | C25H25N5O |
Cas No. | 2102194-04-5 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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